Molecular Imaging of Angiogenesis in Oncology: Current Preclinical and Clinical Status

Angiogenesis is an active process, regulating new vessel growth, and is crucial for the survival and growth of tumours next to other complex factors in the tumour microenvironment. We present possible molecular imaging approaches for tumour vascularisation and vitality, focusing on radiopharmaceuticals (tracers). Molecular imaging in general has become an integrated part of cancer therapy, by bringing relevant insights on tumour angiogenic status. After a structured PubMed search, the resulting publication list was screened for oncology related publications in animals and humans, disregarding any cardiovascular findings. The tracers identified can be subdivided into direct targeting of angiogenesis (i.e., vascular endothelial growth factor, laminin, and fibronectin) and indirect targeting (i.e., glucose metabolism, hypoxia, and matrix metallo-proteases, PSMA). Presenting pre-clinical and clinical data of most tracers proposed in the literature, the indirect targeting agents are not 1:1 correlated with angiogenesis factors but do have a strong prognostic power in a clinical setting, while direct targeting agents show most potential and specificity for assessing tumour vascularisation and vitality. Within the direct agents, the combination of multiple targeting tracers into one agent (multimers) seems most promising. This review demonstrates the present clinical applicability of indirect agents, but also the need for more extensive research in the field of direct targeting of angiogenesis in oncology. Although there is currently no direct tracer that can be singled out, the RGD tracer family seems to show the highest potential therefore we expect one of them to enter the clinical routine.

Lycopene inhibits angiogenesis in human umbilical vein endothelial cells and rat aortic rings

Angiogenesis is important for tumour vascularisation and growth, and is therefore a promising target for cancer therapy. The present study reports inhibition ofin vitroangiogenesis in human umbilical vein endothelial cells (HUVEC) as well as in rat aortic rings at physiological concentrations of lycopene, that is, 1–2 μmol/l. At a final concentration of 1·15 μmol/l, a significant reduction (P < 0·05) in network branching, that is, junction numbers, the number of tubules and tubule length, was observed in both HUVEC as well as in the rat aortic rings. The inhibitory effect of lycopene was independent of the presence of the pro-angiogenic agents, vascular endothelial growth factor and TNF-α. The anti-angiogenic effects of lycopene in the present study were shown at a concentration that should be achievable by dietary means. These results extend our knowledge of one of the putative anti-cancer actions of lycopene.